摘要

An efficient, two-step synthetic strategy has been developed to access the quinolone, naphthyridone and benzonaphthyridone classes of chemotherapeutic agents from Baylis-Hillman adducts. The method involves tandem aza-Michael addition, SNAr cyclisation followed by oxidation of the resulting 4-hydroxy-1,2,3,4-tetrahydroquinoline or 4-hydroxy-1,2,3,4-tetrahydro-1,8-naphthyridine derivative using IBX, and works well with substrates having a wide variety of substitution pattern.

  • 出版日期2014-11-24